CPI-1612 | EP300/CBP inhibitor | Probechem Biochemicals

Chemical Structure : CPI-1612

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CPI-1612 (CPI 1612)

货号: PC-72165Not For Human Use, Lab Use Only.

CPI-1612 (CPI 1612) is a highly potent, selective, orally bioavailable EP300/CBP histone acetyltransferase inhibitor with IC50 of 8.1 nM (EP300 HAT SPA).

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生物&药学活性

CPI-1612 (CPI 1612) is a highly potent, selective, orally bioavailable EP300/CBP histone acetyltransferase inhibitor with IC50 of 8.1 nM (EP300 HAT SPA).
CPI-1612 displays no inhibitory activity in a panel of seven HAT targets (Tip60, HAT1, PCAF, MYST2, MYST3, MYST4, and GCN5L2) and had minimal activity against the antitargets in the Eurofins Safety44 off-target screening panel.
CPI-1612 inhibits JEKO-1 cell growth with GI50 of <7.9 nM, and H3K18Ac MSD EC50 of 14 nM.
CPI-1612 reduced the histone acetylation H3K18Ac in vivo at the primary chromatin acetylation targets of EP300/CBP in a dose- and time-dependent manner.
CPI-1612 showed 67% tumor growth inhibition (TGI) at a dose of 0.5 mg/kg PO BID with concomitant reduction of H3K27Ac in plasma and reduction of H3K18Ac in the tumor.

物理化学性质&存储条件

分子量	450.546
分子式	C27H26N6O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-2-(((S)-2-(4-Cyanophenyl)propyl)amino)-N-(5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-yl)-2-phenylacetamide

参考文献

1. Jonathan E Wilson, et al. ACS Med Chem Lett. 2020 Apr 23;11(6):1324-1329.

CPI-1612 (CPI 1612)

生物&药学活性

物理化学性质&存储条件

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CPI-1612 (CPI 1612)

生物&药学活性

物理化学性质&存储条件

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